Epilepsy refers to the many types of recurrent seizures produced by paroxysmal excessive neuronal discharges in the brain. The mainstay of treatment has been the long-term and consistent administration of anticonvulsant drugs. Unfortunately, despite the many available chemotherapeutic agents, none are capable of achieving total seizure control and most have disturbing effects. Medication remains essentially non-specific and is directed against mechanisms of neuronal hyperexcitability that are poorly understood. Clearly current therapy has not "seized control" of this debilitating disease, rather the reverse still remains true. Recent pharmacological studies support the concept that incorporation of a vicinal diamino-moiety within a substrate is usually accompained by increased CNS depressant activity. Currently, few methods of generality exist for preparation of this group. We are elaborating two new, general, and regiospecific synthetic methods for the construction of a diamino-moiety within the framework of readily accessible starting materials. We are also preparing a select series of derivatives which have incorporated those functional groups which have proven effective in the control of epileptic seizures. The overall criteria for success is the development of new anticonvulsant agents which have high specificity and low toxicity. Samples are being submitted to the National Institutes of Health Epilepsy Branch screening program for evaluation.